journal
MENU ▼
Read by QxMD icon Read
search

European Journal of Drug Metabolism and Pharmacokinetics

journal
https://www.readbyqxmd.com/read/28078530/evaluation-of-the-population-pharmacokinetic-properties-of-lidocaine-and-its-metabolites-after-long-term-multiple-applications-of-a-lidocaine-plaster-in-post-herpetic-neuralgia-patients
#1
Roberta Bursi, Chiara Piana, Joachim Grevel, Dymphy Huntjens, Irmgard Boesl
BACKGROUND AND OBJECTIVES: Lidocaine 5% medicated plaster is the first lidocaine containing product for chronic use. As no previous investigations have been conducted to evaluate the population pharmacokinetics of long-term exposure to lidocaine 5% medicated plasters, further insights into the evaluation of the pharmacokinetic properties of lidocaine and its metabolites were needed for the assessment of its safety. METHODS: The population pharmacokinetic properties of lidocaine and its metabolites were evaluated after multiple applications of lidocaine 5% medicated plasters based on data collected for up to 14...
January 12, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28070880/on-the-molecular-basis-underlying-the-metabolism-of-tapentadol-through-sulfation
#2
Ahsan F Bairam, Mohammed I Rasool, Katsuhisa Kurogi, Ming-Cheh Liu
BACKGROUND AND OBJECTIVES: Previous studies reported that tapentadol-sulfate represented one of the major metabolites of tapentadol excreted in urine. The current study aimed to identify the human cytosolic sulfotransferases (SULTs) that is(are) capable of sulfating tapentadol and to examine whether human cells and human organ specimens are capable of sulfating tapentadol. METHODS: Thirteen human SULTs, previously expressed and purified, as well as human organ cytosols, were analyzed for tapentadol-sulfating activity using an established sulfotransferase assay...
January 10, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28070879/a-review-of-pharmacogenetics-of-antimalarials-and-associated-clinical-implications
#3
REVIEW
Hazem Elewa, Kyle John Wilby
Genetic variability in drug-metabolizing enzymes and drug transporters is known to influence the pharmacokinetics of many drugs. Antimalarial drugs are a class of agents known to utilize metabolic and elimination pathways prone to genetic variation. This paper aims to review the genetic variants affecting antimalarial medications and discuss their clinical implications. Data were identified for the genes coding for the cytochrome P450 (CYP) enzymes: CYP2C8, CYP2C19, CYP2A6, CYP2D6, CYP2B6, and the P-glycoprotein drug transporter...
January 9, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28070878/effects-of-caffeic-acid-and-quercetin-on-in-vitro-permeability-metabolism-and-in-vivo-pharmacokinetics-of-melatonin-in-rats-potential-for-herb-drug-interaction
#4
Snehasis Jana, Himanshu Rastogi
BACKGROUND AND OBJECTIVES: Melatonin is a popular dietary supplement and also considered as pharmaceutical product for sleep disorders. Caffeic acid and quercetin are widely distributed in leafy vegetables, fruits, tea extract, and both are used as natural antioxidant. There is an immense concern for health researchers to study the herb/food-drug interactions of melatonin. It is mainly metabolized by CYP1A2 in human so that herbs/foods containing cytochrome P450 (CYP) inhibitors can affect pharmacokinetics of melatonin...
January 9, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28064419/pharmacokinetics-and-pharmacogenetics-of-carbamazepine-in-children
#5
Natasa Djordjevic, Slobodan M Jankovic, Jasmina R Milovanovic
Although carbamazepine is one of the oldest anticonvulsant drugs, it is still heavily utilized for treatment of epilepsy in children. The aim of this article was to review the current knowledge about pharmacokinetics and pharmacogenetics of carbamazepine in children. The literature for this review was systematically searched for in the MEDLINE and SCINDEKS databases. Oral bioavailability of carbamazepine in children is about 75-85%, and it is approximately 75-85% bound to plasma proteins. Apparent volume of distribution is 1...
January 7, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28064418/novel-antiretroviral-drugs-in-patients-with-renal-impairment-clinical-and-pharmacokinetic-considerations
#6
Dario Cattaneo, Cristina Gervasoni
Highly active antiretroviral therapy (HAART) has dramatically increased the survival of HIV-infected patients from Western countries reducing the incidence of opportunistic infections and AIDS-related malignancies, and improving the patients' quality of life compared with the pre-HAART era. HIV is thus now considered in the West as a chronic disease, with the majority of HIV-infected patients successfully reaching an optimal immune and virological outcome a few months after starting HAART. However, this switch from acute to chronic disease has been accompanied by an increased incidence of chronic kidney disease (CKD), reported in up to 60% of HIV-infected patients...
January 7, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28012025/antifibrotic-effects-of-carvedilol-and-impact-of-liver-fibrosis-on-carvedilol-pharmacokinetics-in-a-rat-model
#7
Ebtehal El-Demerdash, Somaia A Abdel-Sattar, Wesam M El-Bakly, Eman A Mohamed
BACKGROUND AND OBJECTIVES: Carvedilol is a drug of choice in treatment of portal hypertension. The present study was designed to elucidate the potential role of antifibrotic effects of carvedilol in improving hepatic efficiency and the carvedilol oral pharmacokinetic changes during induction of liver fibrosis. METHODS: Rats were given CCl4 (1 ml/kg, intraperitoneal) twice weekly for 6 weeks and/or co-treated with carvedilol (10 mg/kg, orally) three times weekly on alternating days...
December 23, 2016: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28000173/in-vitro-evaluation-of-absorption-characteristics-of-peramivir-for-oral-delivery
#8
Ying Li, Zhiyuan Wang, Xin Li, Wei Gong, Xiangyang Xie, Yang Yang, Wu Zhong, Aiping Zheng
BACKGROUND AND OBJECTIVE: Peramivir is a novel antiviral agent approved for the treatment of severe influenza. However, the development of oral formulation of peramivir has been severely hurdled by poor bioavailability (human, ≤3%). The present work aims to evaluate oral permeability characteristics of peramivir. METHODS: In vitro gastrointestinal stability, metabolic stability in human intestinal S9 fraction and Caco-2 permeability were performed. The liquid chromatography with tandem mass spectrometric (LC-MS/MS) was used to quantify peramivir in buffer and biological sample...
December 21, 2016: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27928655/in-vivo-pharmacokinetics-of-puerarin-via-different-drug-administration-routes-based-on-middle-cerebral-artery-occlusion-model
#9
Pengyue Li, Jie Bai, Boyu Dong, Yang Lu, Shengwei Zhang, Shuang Guo, Ning Tan, Mengdi Zhao, Shouying Du, Puning Cao
BACKGROUND AND OBJECTIVES: Pueraria labata has traditionally been applied in the treatment of stroke in Chinese clinics. Puerarin is the key ingredient in it for brain protection effect. To find a superior administration route for puerarin in the treatment of ischemic cerebrovascular disease, the pharmacokinetics of puerarin based on the middle cerebral artery occlusion (MCAO) rat via different administration routes were studied and compared. METHODS: Ten rats (MCAO model) divided into two groups were treated with puerarin via intravenous and intranasal routes...
December 7, 2016: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27889876/population-pharmacokinetic-pharmacodynamic-modeling-of-5-fluorouracil-for-toxicities-in-rats
#10
Shinji Kobuchi, Yukako Ito, Toshiyuki Sakaeda
BACKGROUND AND OBJECTIVES: Myelosuppression is a dose-limiting toxicity of 5-fluorouracil (5-FU). Predicting the inter- and intra-patient variability in pharmacokinetics and toxicities of 5-FU may contribute to the individualized medicine. This study aimed to establish a population pharmacokinetic-pharmacodynamic model that could evaluate the inter- and intra-individual variability in the plasma 5-FU concentration, 5-FU-induced body weight loss and myelosuppression in rats. METHOD: Plasma 5-FU concentrations, body weight loss, and blood cell counts in rats following the intravenous administration of various doses of 5-FU for 4 days were used to develop the population pharmacokinetic-pharmacodynamic model...
November 26, 2016: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27864798/pharmacokinetic-drug-interactions-with-panax-ginseng
#11
REVIEW
Meenakshi R Ramanathan, Scott R Penzak
Panax ginseng is widely used as an adaptogen throughout the world. The major active constituents of P. ginseng are ginsenosides. Most naturally occurring ginsenosides are deglycosylated by colonic bacteria to intestinal metabolites. Ginsenosides along with these metabolites are widely accepted as being responsible for the pharmacologic activity and drug interaction potential of ginseng. Numerous preclinical studies have assessed the influence of various ginseng components on cytochrome P450 (CYP), glucuronidation, and drug transport activity...
November 18, 2016: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27858342/physiologically-based-pharmacokinetic-pbpk-modeling-of-pitavastatin-and-atorvastatin-to-predict-drug-drug-interactions-ddis
#12
Peng Duan, Ping Zhao, Lei Zhang
BACKGROUND: The disposition of statins varies and involves both metabolizing enzymes and transporters, making predictions of statin drug-drug interactions (DDIs) challenging. Physiologically based pharmacokinetic (PBPK) models have, however, demonstrated ability to predict complex DDIs. OBJECTIVE: In this study, PBPK models of two statins (pitavastatin and atorvastatin) were developed and applied to predict pitavastatin and atorvastatin associated DDIs. METHOD: Pitavastatin and atorvastatin PBPK models were developed using in vitro and human pharmacokinetic data in a population-based PBPK software (SimCYP(®)) by considering the contribution of both metabolizing enzymes and transporters to their overall pharmacokinetics...
November 17, 2016: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27853934/evaluation-of-in-vitro-cytochrome-p450-inhibition-and-in-vitro-fate-of-structurally-diverse-n-oxide-metabolites-case-studies-with-clozapine-levofloxacin-roflumilast-voriconazole-and-zopiclone
#13
Poonam Giri, Sneha Naidu, Nirmal Patel, Harilal Patel, Nuggehally R Srinivas
BACKGROUND AND OBJECTIVES: The role of metabolite(s) to elicit potential clinical drug-drug interaction (DDI) via cytochrome P450 enzymes (CYP) is gaining momentum. In this context, the role of N-oxides for in vitro CYP inhibition has not been evaluated. The objectives of this study were: (a) to examine in vitro CYP inhibition of N-oxides of clozapine, levofloxacin, roflumilast, voriconazole and zopiclone in a tiered approach and (b) evaluate in vitro fate of aforementioned N-oxides examined in recombinant CYPs, human microsomes and hepatocytes...
November 16, 2016: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27815731/hepatic-uptake-mechanism-of-ophiopogonin-d-mediated-by-organic-anion-transporting-polypeptides
#14
Wen Zhang, Xiaomin Xiong, Lin Chen, Mingyi Liu, Yuqing Xiong, Hong Zhang, Shibo Huang, Chunhua Xia
BACKGROUND AND OBJECTIVES: Ophiopogonin D (OPD) is one of the main active ingredients of SMI (Shenmai injection) which is widely used in clinical practice in China. Our previous study indicated  that OPD might be transported from blood into liver mediated by organic anion transporting polypeptides (OATPs/oatps). This study aims to explore the hepatic uptake mechanism of OPD in rat and human. METHODS: Rosuvastatin (a competitive inhibitor of oatp1b2, oatp1a1, and oatp1a4), glycyrrhizic acid (a specific inhibitor of oatp1b2), digoxin (a specific inhibitor of oatp1a4), bromosulfophthalein (BSP), and ibuprofen (a specific inhibitor of oatp1a1) were used to study the uptake of OPD in rat hepatocytes...
November 4, 2016: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27778300/liver-perfusion-modifies-gd-dtpa-and-gd-bopta-hepatocyte-concentrations-through-transfer-clearances-across-sinusoidal-membranes
#15
Jean-Luc Daire, Benjamin Leporq, Valérie Vilgrain, Bernard E Van Beers, Sabine Schmidt, Catherine M Pastor
BACKGROUND AND OBJECTIVES: Gadobenate dimeglumine (Gd-BOPTA) is a commercialised hepatobiliary contrast agent used during liver magnetic resonance imaging (MRI) to detect liver diseases. It enters into human hepatocytes through organic anion transporting polypeptides (OATP1B1/B3) and crosses the canalicular transporter multiple resistance-associated protein 2 (MRP2) to be excreted into bile canaliculi. Gd-BOPTA can return to sinusoids via the sinusoidal transporters MRP3/MRP4. Hepatocyte concentrations of Gd-BOPTA depend on three clearances: the sinusoidal clearance or volume of sinusoidal blood cleared of drugs per unit of time and two hepatocyte clearances (into bile canaliculi or back to sinusoids) or volume of hepatocytes cleared of drugs per unit of time in the respective liver compartments...
October 24, 2016: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27848195/acknowledgements
#16
(no author information available yet)
No abstract text is available yet for this article.
December 2016: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27278683/interaction-of-citrus-juices-with-cyclosporine-systematic-review-and-meta-analysis
#17
REVIEW
Kannan Sridharan, Gowri Sivaramakrishnan
INTRODUCTION: Cyclosporine is an immunosuppressant with narrow therapeutic window, metabolized mainly by cytochrome P450 3A4 (CYP3A4) and minimally by cytochrome P450 3A5 (CYP3A5). Citrus juices such as grapefruit juice (GFJ), orange, lemon, pomelo and lime were known to interact with cyclosporine in several randomized controlled trials. The present review is a systematic compilation and quantitative synthesis on the changes of cyclosporine pharmacokinetics with concomitant citrus juice administration...
December 2016: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27233798/proposing-the-use-of-partial-auc-as-an-adjunctive-measure-in-establishing-bioequivalence-between-deltoid-and-gluteal-administration-of-long-acting-injectable-antipsychotics
#18
Lik Hang N Lee, Charles Choi, Pavel Gershkovich, Alasdair M Barr, William G Honer, Ric M Procyshyn
The maximum plasma concentration (C max) and the area under the plasma concentration-time curve (AUC) are commonly used to establish bioequivalence between two formulations of the same oral medication. Similarly, these pharmacokinetic parameters have also been used to establish bioequivalence between two sites of administration for the same injectable formulation. However, these conventional methods of establishing bioequivalence are of limited use when comparing modified-release formulations of a drug, particularly those with rates of absorption that are amenable to change with the site of injection...
December 2016: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/26650374/effect-of-ginkgo-leaf-tablets-on-the-pharmacokinetics-of-amlodipine-in-rats
#19
Rong Wang, Hai Zhang, Sen Sun, Yuanyuan Wang, Yifeng Chai, Yongfang Yuan
BACKGROUND AND OBJECTIVE: Ginkgo leaf tablet (GLT) is an effective traditional Chinese multi-herbal formula, which is often combined with amlodipine for treating senile hypertension in clinic. The aim of this study was to study the pharmacokinetics of amlodipine after oral administration of amlodipine and GLT and to investigate the potential for pharmacokinetic herb-drug interactions between GLT and amlodipine in rats. METHODS: A liquid chromatography-tandem mass spectrometry (LC-MS/MS) analytical method was developed for quantification of amlodipine in rat plasma...
December 2016: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/26628429/presence-of-an-h-quinidine-antiport-system-in-madin-darby-canine-kidney-cells
#20
Miki Fukao, Eri Kondo, Hiroki Nishino, Ryutaro Hattori, Asuka Horie, Yukiya Hashimoto
BACKGROUND AND OBJECTIVES: We have recently found an H(+)/quinidine antiport system in human kidney HEK 293 cells. The aim of the present study was to evaluate whether the H(+)/quinidine antiport system is expressed in Madin-Darby canine kidney (MDCK) cells. METHODS: We investigated the uptake and efflux of quinidine in MDCK cells. RESULTS: The uptake of 100 µM quinidine into MDCK cells was decreased by acidification of extracellular pH or alkalization of intracellular pH...
December 2016: European Journal of Drug Metabolism and Pharmacokinetics
journal
journal
26770
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"